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Literature summary for 2.4.1.80 extracted from

  • Aerts, J.M.; Ottenhoff, R.; Powlson, A.S.; Grefhorst, A.; van Eijk, M.; Dubbelhuis, P.F.; Aten, J.; Kuipers, F.; Serlie, M.J.; Wennekes, T.; Sethi, J.K.; ORahilly, S.; Overkleeft, H.S.
    Pharmacological inhibition of glucosylceramide synthase enhances insulin sensitivity (2007), Diabetes, 56, 1341-1349.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine it is shown that pharmacological lowering of glycosphingolipids, without significant reduction of ceramide, dramatically reverses insulin resistance in in vitro and in vivo models and may present a novel approach to the therapy of type 2 diabetes Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
N-(5'-adamantan-1'-yl-methoxy)-pentyl-1-deoxynojirimycin highly specific small molecule inhibitor of glucosylceramide synthase. When administered to mice and rats, it significantly reduces glycosphingolipid but not ceramide concentrations in various tissues. Treatment of ob/ob mice with the inhibitor normalizes their elevated tissue glucosylceramide levels, markedly lowers circulating glucose levels, improves oral glucose tolerance, reduced A1C, and improves insulin sensitivity in muscle and liver Mus musculus
N-(5'-adamantane-1'-yl-methoxy)-pentyl-1-deoxynojirimycin pharmacological inhibition of glucosylceramide synthase enhances insulin sensitivity Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-glucose + N-acylsphingosine Mus musculus the enzyme catalyzes a necessary step in the conversion of ceramide to glycosphingolipids UDP + D-glucosyl-N-acylsphingosine
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?

Organism

Organism UniProt Comment Textmining
Mus musculus
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Source Tissue

Source Tissue Comment Organism Textmining
3T3-L1 cell
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Mus musculus
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NIH-3T3 cell
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Mus musculus
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-glucose + N-acylsphingosine the enzyme catalyzes a necessary step in the conversion of ceramide to glycosphingolipids Mus musculus UDP + D-glucosyl-N-acylsphingosine
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?

Synonyms

Synonyms Comment Organism
GCS
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Mus musculus
glucosylceramide synthase
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Mus musculus